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Proceedings of the National Academy of Sciences of the United States of America logoLink to Proceedings of the National Academy of Sciences of the United States of America
. 1995 Mar 28;92(7):2775–2779. doi: 10.1073/pnas.92.7.2775

Benzodiazepine receptors mediate regional blood flow changes in the living human brain.

E Matthew 1, P Andreason 1, K Pettigrew 1, R E Carson 1, P Herscovitch 1, R Cohen 1, C King 1, C E Johanson 1, D J Greenblatt 1, S M Paul 1
PMCID: PMC42301  PMID: 7708722

Abstract

We studied the effects of a high-affinity gamma-aminobutyric acid (GABA)-benzodiazepine-receptor agonist (lorazepam) and an antagonist (flumazenil) in humans, using H2(15)O positron-emission tomography. Administration of lorazepam to healthy volunteers caused time- and dose-dependent reductions in regional cerebral blood flow and self-reported alterations in behavioral/mood parameters. Flumazenil administration reversed these changes. These observations indicated that benzodiazepine-induced effects on regional cerebral blood flow and mood/behavior are mediated at some level through GABA-benzodiazepine receptors, although the specific mechanism remains unclear. The approach described here provides a method for quantifying GABA-benzodiazepine-receptor-mediated neurotransmission in the living human brain and may be useful for studying the role of these receptors in a variety of neuropsychiatric disorders.

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